Taxol derivatives, their preparation and pharmaceutical compositions containing them

• US 4,814,470 A
• Filed: 07/14/1987
• Issued: 03/21/1989
• Est. Priority Date: 07/17/1986
• Status: Expired due to Term

• Current Assignee: Aventis Pharma SA (Sanofi )
• Original Assignee: Rhone-Poulenc Sante (Sanofi )
• Inventors: Gueritte-Voegelein, Francoise, Colin, Michel, Potier, Pierre, Guenard, Daniel
• Primary Examiner(s): Hollrah, Glennon H.
• Assistant Examiner(s): Russell, Mark W.
• Application Number:
  US07/073,156
• Time in Patent Office: 616 Days
• Field of Search: 549/510, 514/449
• US Class Current: 514/449
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: C07D 305/14 condensed with carbocyclic rings or ring systems

Abstract

Taxol derivatives of formula ##STR1## in which R represents hydrogen or acetyl, one of R₁ or R₂ represents hydroxy and the other represents tert-butoxycarbonylamino and their isomers are useful antitumor agents.

Claims

1. A taxol derivative of formula:

##STR7## in which R represents hydrogen or acetyl and one of R₁ and R₂ represents hydroxy and the other represents tert-butoxycarbonylamino, and the stereoisomeric forms thereof and their mixtures.

2. A taxol derivative according to claim 1, in which R is hydrogen, R₁ is hydroxy and R₂ is tert-butoxycarbonylamino, and having the 2'"'"'R, 3'"'"'S configuration.

3. A taxol derivative according to claim 1, in which R is hydrogen, R₁ is hydroxy, and R₂ is tert-butoxycarbonylamino, and having the 2'"'"'S, 3'"'"'R configuration.

4. A taxol derivative according to claim 1, in which R is hydrogen, R₁ is tert-butoxycarbonylamino, and R₂ is hydroxy, and having the 2'"'"'R, 3'"'"'S configuration.

5. A taxol derivative according to claim 1, in which R is hydrogen, R₁ is tert-butoxycarbonylamino, and R₂ is hydroxy and having the 2'"'"'S, 3'"'"'R configuration.

6. A pharmaceutical composition which contains a taxol derivative as claimed in claim 1 combined with one or more pharmaceutically acceptable, inert or physiologically active diluents or adjuvants.